新型免疫抑制剂FTY-720的合成

分别以苯为原料, 经傅克酰基化、 还原、 酰化、 缩合、 还原羰基、 还原酯基、 去乙酰化、 成盐反应和以苯乙醇为原料, 经氯化、 傅克酰基化、 缩合、 还原羰基、 还原酯基、 去乙酰化、 成盐反应合成目标分子FTY-720, 总收率分别为17%和21%. 各关键中间体及FTY-720的结构经红外光谱、 核磁共振氢谱及碳谱、 质谱等得到确证.

Synthesis of a New Immunosuppressant FTY-720

FTY-720, a new kind of immunosuppressant, 2-amino 2-［2-(4-octylphenyl)ethyl-1,3-propanediol hydrochloride was synthesized via Friedel crafts acylation, reduction, acylation, alkylation and Et₃SiH/ TiCl₄ reduction as a pivotal step from the starting material benzene or Friedel crafts acylation, alkylation, Et₃SiH/ TiCl₄ reduction and reduction as a pivotal step from the starting material phenethyl alcohol respectively and the total yield of the FTY-720 was 17% or 21% respectively. The structure of the target molecule and the key intermediates were confirmed by IR, ¹H NMR, ¹³C NMR and MS in our experiments. The route is simpler, more efficientand convenient that may be applied to industrial production.